专利号:US-7002006-B2 优先权日:2003-02-12 标 题:Protection of nucleosides 发明人:SONG QUANLAI; ROSS BRUCE S 权利人:ISIS PHARMACEUTICALS INC 摘要:A process of manufacturing protected nucleosides comprises reacting a nucleoside with a protecting reagent in the presence of a regioselective activator to produce a regioselectively protected nucleoside. In some embodiments of the inventive method, an optionally substituted trityl or optionally substituted pixyl group is selectively added to the 5'-O-position of a nucleoside in the presence of lutidine as activator or activator/solvent. The inventive method results in improved selectivity of the 5'-O-position over the 3'-O-position, thereby improving overall product yield and purity, and permitting simplified purification protocols, in some cases obviating the need for chromatography to produce a purified protected nucleoside suitable for automated synthesis of oligonucleotides, such as primers, probes and antisense molecules.
专利号:US-2015139987-A1 优先权日:2013-11-20 标 题 :Treatment of homozygous familial hypercholesterolemia 发明人:MARTIN ROBERT L; MCWHERTER CHARLES A; O'MARA PATRICK J 权利人:CYMABAY THERAPEUTICS INC 摘要:Treatment of homozygous familial hypercholesterolemia by administration of (R)-2-(4-((2-ethoxy-3-(4-(trifluoromethyl)phenoxy)propyl)thio)-2-methylphenoxy)acetic acid or a salt thereof, optionally in combination with an MTP inhibitor, an apoB-100 synthesis inhibitor, or a PCSK9 inhibitor.
专利号:US-12338436-B2 优先权日:2018-06-29 标题 :Synthetic guide molecules, compositions and methods relating thereto 发明人:SACCOMANO SAM; CAPEHART STACY; EATON BRUCE; BERRY KARIN ZEMSKI 权利人:EDITAS MEDICINE INC 摘要:Chemical syntheses of guide molecules are disclosed, along with compositions and methods relating thereto. A cost-effective and straightforward chemical synthesis of high-purity unimolecular guide molecules with minimal n−1 and/or n+1 species, truncation species, and other contaminants by providing, among other things, methods for synthesizing unimolecular guide molecules that involve cross-linking two or more pre-annealed guide fragments.
专利号:CN-118047824-A 优先权日:2024-04-01 标 题:Application of dialkylphosphonic acid in oligonucleotide synthesis
专利号:CN-118047824-B 优先权日:2024-04-01 标题 :Application of dialkylphosphonic acid in oligonucleotide synthesis
参考标题:Protection Of Nucleosides 摘要:A Process Of Manufacturing Protected Nucleosides Comprises Reacting A Nucleoside With A Protecting Reagent In The Presence Of A Regioselective Activator To Produce A Regioselectively Protected Nucleoside. In Some Embodiments Of The Inventive Method, An Optionally Substituted Trityl Or Optionally Substituted Pixyl Group Is Selectively Added To The 5′-O-Position Of A Nucleoside In The Presence Of Lutidine As Activator Or Activator/solvent. The Inventive Method Results In Improved Selectivity Of The 5′-O-Position Over The 3′-O-Position, Thereby Improving Overall Product Yield And Purity, And Permitting Simplified Purification Protocols, In Some Cases Obviating The Need For Chromatography To Produce A Purified Protected Nucleoside Suitable For Automated Synthesis Of Oligonucleotides, Such As Primers, Probes And Antisense Molecules.